Method for preparing a solid sustained release form of a functionally active composition

Abstract

PCT No. PCT US88/04208 Sec. 371 Date Apr. 26, 1990 Sec. 102(e) Date Apr. 26, 1990 PCT Filed Nov. 23, 1988.The invention is a sustained release dosage or delivery form, such as a tablet, pill, granule or the like capable of providing sustained release of a functionally active ingredient and the method for its manufacture. The invention comprises a matrix of a polymer containing functionally active ingredient and an excipient shaped at or above the glass transition temperature of said polymer into a form such as a granule, tablet or the like. Preferably the excipient is a microcrystalline cellulose.

We claim: 
     
       1. A method for preparing a sustained release dosage form comprising blending into a feed formulation a dosage amount of a functionally active ingredient, an excipient and a polymer or copolymer having a glass transition temperature of about 30° C. to about 150° C., said polymer being present in sufficient quantity to provide from 5% to 50% polymer or copolymer, 1% to 90% excipient, and from 5% to 90% of the functionally active ingredient in the dosage form, processing at least part of the feed formulation into a shaped form and maintaining the shaped form at or above the glass transition temperature of the polymer for from 1 to 12 hours to provide a dosage form having controlled, sustained release of the functionally active ingredient when the dosage form is administered. 
     
     
       2. A method for preparing a sustained release dosage form comprising blending into a feed formulation a dosage amount of a functionally active ingredient, an excipient and a polymer having a glass transition temperature of 30° C. to 150° C. selected from the group consisting of polyisobutylene, polymers and copolymers of acrylic acid, methacrylic acid, hydroxyalkylacrylic acid, hydroxyalkylmethacrylic acid and their methyl, ethyl and lauryl esters, poly(ethylene oxide), cellulose acetate, cellulose acetate butyrate, cellulose acetate proprionate, ethyl cellulose, polyesters of polyhydric alcohols and dicarboxylic acids, polyethers, cellulose acetate phthalate, dl-polylactic acid, polyglycolic acid, polylactic-polyglycolic copolymers, polycaprolactone, polhydroxybutyrate, polyhydroxyvalerate and polyethylene glycols, mixtures and copolymers thereof to provide from 5% to 50% polymer or copolymer, 1% to 90% excipient and 5% to 90% of the functionally active ingredient processing at least part of the feed formulation into a shaped form characterized by maintaining the shaped form at or above the glass transition temperature of the polymer for from 1 to 12 hours to provide a dosage form having controlled, sustained release of the functionally active ingredient when the dosage form is administered in the dosage form. 
     
     
       3. The sustained release dosage form of claim 1 or 2 characterized in that the polymer or copolymer has a glass transition temperature of 40° C. to 100° C. 
     
     
       4. The sustained release dosage form of claims 1 or 2 characterized in that the excipient is selected from the group consisting of lactose, dicalcium phosphate, calcium sulfate, sugar, microcrystalline cellulose, gums, methylcellulose, starch, polyvinylpyrrolidone and clay. 
     
     
       5. The sustained release dosage form of claim 4 characterized in that the form is a tablet, bead, microcapsule, pill or a granule. 
     
     
       6. The sustained release dosage form of claim 4 characterized in that the pharmaceutically active ingredient is selected from the group consisting of theophylline, quinidine sulfate, propranolol, chlorpheniramine, testosterone and ethenyl estradiol.